Drug intelligence / Profile preview

WBC100

Development stage
Phase 1
Lead developer
Weben Pharma
Modality
Molecular Glues → Targeted Protein Degraders (TPDs) → Small Molecules
Administration
Oral
01

Overview

WBC100 is a novel, potent, orally active small molecule that functions as a molecular glue degrader specifically targeting the c-Myc oncoprotein. It binds to the nuclear localization signal 1 (NLS1)–Basic–nuclear localization signal 2 (NLS2) region of c-Myc and induces its degradation via the ubiquitin E3 ligase CHIP-mediated 26S proteasome pathway. This targeted degradation leads to apoptosis in cancer cells that overexpress c-Myc. Preclinical studies have shown that WBC100 potently regresses multiple lethal c-Myc overexpressing tumors—including acute myeloid leukemia, pancreatic cancer, and gastric cancer—with good tolerability in xenograft mouse models. The drug is currently being evaluated in phase I clinical trials for relapsed or refractory acute myeloid leukemia and advanced solid tumors with high c-Myc expression[2][4][5][6].

Other names
14-D-Valine-TPL
02

Targets

STUB1 (E3 ubiquitin-protein ligase CHIP)MYC (MYC proto-oncogene protein)

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